The Application of Click Chemistry In Life Sciences

CHANGSHA, China - March 24, 2021 - PRLog -- Click chemistry has come into its own in a wide range of life science applications and opens up opportunities that lie between chemistry, biology and material science.

What is click chemistry?

Click chemistry is modular, wide in scope, gives very high reaction yields and generates only harmless by-products. Ideally insensitive to water and oxygen, the reaction conditions are benign, and the product requires little downstream purification.

This would have excluded classic reactions like the Huisgen cycloaddition of an alkyne and an azide, which is useful for linking molecules, as traditionally this reaction requires refluxing in an organic solvent at 100˚C and still produces a mixture of isomer products.

However, the addition of copper as a catalyst transforms the reaction into a prime example of click chemistry, by speeding up the reaction at lower temperature and favouring the formation of only one product.

Yet, even trace amounts of copper can be difficult to remove and harmful to cells. A copper-free click reaction was created by adding ring strains — akin to 'loaded springs' — to the click reactants. Releasing such strain becomes the driving force for the reaction, which readily proceeds at room temperature and without the metal catalyst.

With progress in catalysts and the utilisation of ring strains, many classic chemical reactions have been reinvented as click chemistry and can now be carried out at ambient temperatures and under conditions that are harmless to living organisms and biological molecules.

These attributes make click chemistry particularly appealing for bioconjugation, where biocompatible, highly specific and non-toxic chemical strategies are required to join together two or more molecules, one of which is a biomolecule.

Click chemistry in life science applications

Click chemistry is already widely used in pharmaceutical and life science applications and increasingly prompting large commercial deals.

Drug discovery has been boosted by click chemistry, as not only the resulting chemical linkages (such as the triazole ring) are highly useful in medicinal chemistry, but also new and potentially more active compounds can be formed by clicking existing compounds together. This is seen in fragment-based drug screening and PROTAC, a targeted protein degradation drug platform, which is considered as the next hot drug development area.

In the nucleic acid sequencing arena, ClickSeq, a click chemistry-based method for RNA sequencing has proven to be more robust and less error-prone than the enzymatic ligation commonly used to link sequencing adaptors during the creation of libraries for next-generation Illumina sequencing.

Biochempeg (https://www.biochempeg.com/) is especially good at click chemistry reagents which now widely used on biomolecular probes, two-dimensional gel electrophoresis separation, modification of peptide function with triazoles and natural products, and pharmaceuticals, nanotechnology, Biomaterials, etc.